354517-76-3Relevant academic research and scientific papers
Novel optimization of valmerins (tetrahydropyrido[1,2- a ]isoindolones) as potent dual CDK5/GSK3 inhibitors
Ouach, Aziz,Boulahjar, Rajaa,Vala, Christine,Bourg, Stéphane,Bonnet, Pascal,Guguen-Guillouzo, Christiane,Ravache, Myriam,Le Guevel, Rémy,Lozach, Olivier,Lazar, Sa?d,Troin, Yves,Meijer, Laurent,Ruchaud, Sandrine,Akssira, Mohamed,Guillaumet, Gérald,Routier, Sylvain
, p. 311 - 325 (2016/04/05)
An efficient synthetic strategy able to modulate the structure of the tetrahydropyridine isoindolone (Valmerin) skeleton was developed. A library of more than 30 novel final structures was generated. Biological activities on CDK5 and GSK3 as well as cellular effects on cancer cell lines were measured for each novel compound. Additionally to support the SAR, a docking study was performed. A potent GSK3/CDK5 dual inhibitor (37, IC50 CDK5/GSK3 35/7 nM) was obtained. Best antiproliferative effects were obtained on lung and prostate cell lines with IC50 Combining double low line 20 nM.
PIPERAZINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLU5 RECEPTORS
-
Page/Page column 74, (2013/07/05)
This invention relates to compounds of formula (I) their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. R1, R2, R3, R4, Q have meanings given in the description.
NOVEL COMPOUNDS
-
Paragraph 0466; 0467; 0468; 0469; 0470, (2013/06/28)
This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. R1, R2, R3, R4, Q have meanings given in the description.
